Ruthenium-Mediated [2+2+2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology
文献类型:期刊论文
作者 | Suo, Yanrui1,2; Xu, Min3; Sun, Meimei1; Lu, Weiwei1; Wang, Xuan1; Lu, Xiaojie1,2![]() |
刊名 | ORGANIC LETTERS
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出版日期 | 2022-12-07 |
页码 | 5 |
ISSN号 | 1523-7060 |
DOI | 10.1021/acs.orglett.2c03759 |
通讯作者 | Wang, Xuan(wangxuan2@simm.ac.cn) ; Lu, Xiaojie(xjlu@simm.ac.cn) |
英文摘要 | Indane and isoindoline are attractive bicyclic systems in biologically active compounds but are rarely reported in DNA-encoded libraries. In this paper, we reported an efficient and versatile approach for assembling indane and isoindoline scaffolds via a ruthenium-catalyzed [2 + 2 + 2] cyclotrimerization reaction. This method exhibits a broad substrate scope and has been successfully applied to construct a 53K-membered DNA-encoded library (DEL). In order to test its application, we carried out a preliminary selection of this DEL against Aurora A protein and identified a hit compound with 9.3 mu M inhibition activity. |
WOS关键词 | CHEMISTRY ; DANOPREVIR ; DISCOVERY ; SELECTION ; DESIGN |
资助项目 | Shanghai Municipal Science and Technology Major Project ; [NSFC-91953203] ; [NSFC-21877117] ; [NSFC-21907103] |
WOS研究方向 | Chemistry |
语种 | 英语 |
WOS记录号 | WOS:000893455600001 |
出版者 | AMER CHEMICAL SOC |
源URL | [http://119.78.100.183/handle/2S10ELR8/304324] ![]() |
专题 | 新药研究国家重点实验室 |
通讯作者 | Wang, Xuan; Lu, Xiaojie |
作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China |
推荐引用方式 GB/T 7714 | Suo, Yanrui,Xu, Min,Sun, Meimei,et al. Ruthenium-Mediated [2+2+2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology[J]. ORGANIC LETTERS,2022:5. |
APA | Suo, Yanrui,Xu, Min,Sun, Meimei,Lu, Weiwei,Wang, Xuan,&Lu, Xiaojie.(2022).Ruthenium-Mediated [2+2+2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology.ORGANIC LETTERS,5. |
MLA | Suo, Yanrui,et al."Ruthenium-Mediated [2+2+2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology".ORGANIC LETTERS (2022):5. |
入库方式: OAI收割
来源:上海药物研究所
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